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1. 发明授权

US08329905B2 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 有权
标题翻译： {[5-（3-氟苯基） - 吡啶-2-基]甲基}膦酸二乙酯的合成
公开(公告)号：US08329905B2
公开(公告)日：2012-12-11
申请号：US12701174
申请日：2010-02-05
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Thiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Thiruvettipuram K. Thiruvengadam
IPC分类号： C07F9/40
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

2. 发明授权

US07687631B2 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 有权
标题翻译： {[5-（3-氟苯基） - 吡啶-2-基]甲基}膦酸二乙酯的合成
公开(公告)号：US07687631B2
公开(公告)日：2010-03-30
申请号：US11824245
申请日：2007-06-29
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

3. 发明申请

US20100137597A1 SYNTHESIS Of DIETHYLPHOSPHONATE 有权
标题翻译：二乙基磷酸酯的合成
公开(公告)号：US20100137597A1
公开(公告)日：2010-06-03
申请号：US12701174
申请日：2010-02-05
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07F9/40
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

4. 发明授权

US07605275B2 Exo- and diastereo- selective syntheses of himbacine analogs 有权
标题翻译：烟草类似物的外切和非对映选择性合成
公开(公告)号：US07605275B2
公开(公告)日：2009-10-20
申请号：US11331324
申请日：2006-01-12
申请人： Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam
发明人： Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07D307/92
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译：本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。本文教导的化学结构可以举例说明如下：

5. 发明申请

US20110092716A1 DEHYDROHALOGENATION PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN PROVIDING 6,6-DIMETHYL-3-AZABICYCLO-[3.1.0]- HEXANE COMPOUNDS 审中-公开
标题翻译：用于制备适用于提供6,6-二甲基-3-氮杂双环[3.1.0] - 六氢化合物的中间体的脱氢脱氢反应方法
公开(公告)号：US20110092716A1
公开(公告)日：2011-04-21
申请号：US12745153
申请日：2008-11-20
申请人： Daw-long Kwok , Hong-Chang Lee , Ilia A. Zavialov
发明人： Daw-long Kwok , Hong-Chang Lee , Ilia A. Zavialov
IPC分类号： C07D209/02
CPC分类号： C07D209/52
摘要： The present invention provides for a process for preparing the pyrrole compounds of Formula Va and Vb.
摘要翻译：本发明提供制备式Va和Vb的吡咯化合物的方法。

6. 发明授权

US07326795B2 Process and intermediates for the preparation of (1R,2S,5S)-3-azabicyclo[3,1,0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[1,1-dimethylethyl]amino]carbonylamino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl 失效
标题翻译：制备（1R，2S，5S）-3-氮杂双环[3,1,0]己烷-2-甲酰胺，N- [3-氨基-1-（环丁基甲基）-2,3-二氧代丙基] -3 - [（2S）-2 - [[[1,1-二甲基乙基]氨基]羰基氨基] -3,3-二甲基-1-氧代丁基] -6,6-二甲基
公开(公告)号：US07326795B2
公开(公告)日：2008-02-05
申请号：US10867600
申请日：2004-06-15
申请人： Anantha Sudhakar , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Orr , Hoa N. Nguyen , Juergen Weber , Ingyu Jeon , Minzhang Chen , Michael D. Green , George S. Wong , Jeonghan Park , Tetsuo Iwama
发明人： Anantha Sudhakar , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Orr , Hoa N. Nguyen , Juergen Weber , Ingyu Jeon , Minzhang Chen , Michael D. Green , George S. Wong , Jeonghan Park , Tetsuo Iwama
IPC分类号： C07D209/52 , C07C233/08
CPC分类号： C07K5/0202 , C07C271/22 , C07C2601/04
摘要： In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.
摘要翻译：在一个实施方案中，本申请涉及制备式I化合物的方法以及在制备式I化合物的方法中制备的某些中间体化合物。

7. 发明授权

US06232467B1 Method for the synthesis of amines and amino acids with organoboron derivatives 失效
标题翻译：用有机硼衍生物合成胺和氨基酸的方法
公开(公告)号：US06232467B1
公开(公告)日：2001-05-15
申请号：US08884188
申请日：1997-06-27
申请人： Nicos A. Petasis , Ilia A. Zavialov
发明人： Nicos A. Petasis , Ilia A. Zavialov
IPC分类号： C07C20900
CPC分类号： C07D295/15 , C07B2200/07 , C07C213/02 , C07C227/10 , C07C231/08 , C07C2603/74 , C07D207/16 , C07D307/52 , C07D333/16 , C07D333/20 , C07D333/24 , C07D333/58 , C07D333/60 , C07H5/06 , C40B40/00 , C07C215/28 , C07C229/36 , C07C233/47
摘要： Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.
摘要翻译：胺和氨基酸通过在温和条件下使胺，羰基衍生物和有机硼化合物反应来制备。

8. 发明申请

US20110251392A1 EXO- AND DIASTEREO- SELECTIVE SYNTHESIS OF HIMBACINE ANALOGS 有权
标题翻译：乙酰胺类似物的外源和二硫选择性合成
公开(公告)号：US20110251392A1
公开(公告)日：2011-10-13
申请号：US13168029
申请日：2011-06-24
申请人： George Wu , Anantha R. Sudhakar , Mingsheng Huang , Tao Wang , Vijay Sabesan , Ji Xie , Frank Xing Chen , Marc Poirier , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie. Lim
发明人： George Wu , Anantha R. Sudhakar , Mingsheng Huang , Tao Wang , Vijay Sabesan , Ji Xie , Frank Xing Chen , Marc Poirier , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie. Lim
IPC分类号： C07F9/141 , C07C205/56 , C07C309/16 , C07D213/02 , C07C235/00 , C07C205/44 , C07D307/77 , C07D277/64
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译：本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。本文教导的化学结构可以举例说明如下：

9. 发明申请

US20090281321A1 EXO- AND DIASTEREO- SELECTIVE SYNTHESES OF HIMBACINE ANALOGS 有权
标题翻译：乙酰胺类似物的外 - 和二选择性合成
公开(公告)号：US20090281321A1
公开(公告)日：2009-11-12
申请号：US12505079
申请日：2009-07-17
申请人： George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
发明人： George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
IPC分类号： C07C69/608 , C07D405/08 , C07F9/40 , C07D307/92 , C07D417/08 , C07D277/64
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译：本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。本文教导的化学结构可以举例说明如下：

10. 发明授权

US06482952B2 Process for preparing acetonides 失效
标题翻译：丙酮化合物的制备方法
公开(公告)号：US06482952B2
公开(公告)日：2002-11-19
申请号：US09883417
申请日：2001-06-18
申请人： Steven J. Cianciosi , Gregory L. Tewalt , Eric T. Pisk , Ilia A. Zavialov , Glenn A. Hulvey
发明人： Steven J. Cianciosi , Gregory L. Tewalt , Eric T. Pisk , Ilia A. Zavialov , Glenn A. Hulvey
IPC分类号： C07D26352
CPC分类号： C07D263/52
摘要： Acetonides are obtained in a one-step reaction of a carboxylic acid halide, a 1,2-aminoalcohol, and 2-alkoxypropene or 2,2-dialkoxypropane in an ether solvent and in the presence of an inorganic base. Acetonides are also obtained in a two-step reaction scheme in which an acid halide and 1,2-aminoalcohol are reacted in an ether solvent in the presence of LiOH to form a hydroxyamide, which is then reacted with 2-alkoxypropene or 2,2-dialkoxypropane in the presence of acid to form the acetonide. The acetonides resulting from the one-step and two-step protocols can be further reacted with an allylating agent such as an allyl halide in the presence of a strong base to provide the corresponding allyl acetonide. The acetonides and allyl acetonides can serve as intermediates in the production of certain HIV protease inhibitors which are useful for treating HIV infection and AIDS.
摘要翻译：在醚溶剂中和无机碱的存在下，在羧酸卤化物，1,2-氨基醇和2-烷氧基丙烯或2,2-二烷氧基丙烷的一步反应中获得乙氧基化物。乙酸酯也是以两步反应方案获得的，其中酰卤和1,2-氨基醇在醚溶剂中在LiOH存在下反应形成羟基酰胺，然后与2-烷氧基丙烯或2,2 二烷氧基丙烷在酸存在下形成丙酮化合物。由一步法和两步法得到的丙酮化合物可以在强碱存在下与烯丙基化剂如烯丙基化物进一步反应，得到相应的烯丙基丙酮化合物。丙酮化合物和烯丙基丙酮化物可用作生产某些可用于治疗艾滋病毒和艾滋病的HIV蛋白酶抑制剂的中间体。

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